Ezlopitant
 | |
| Clinical data | |
|---|---|
| Routes of administration | By mouth |
| ATC code | none |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Excretion | Urine (32%), Feces (51%) |
| Identifiers | |
| |
| Synonyms | CJ-11,974; (2S,3S)-2-Diphenylmethyl-3-[(5-isopropyl-2-methoxybenzyl)amino]quinuclidine[1] |
| CAS Number | 147116-64-1 |
| PubChem (CID) | 188927 |
| IUPHAR/BPS | 5751 |
| ChemSpider | 164166 |
| UNII |
3L098A8MPY  |
| ChEMBL | CHEMBL515966 |
| Chemical and physical data | |
| Formula | C31H38N2O |
| Molar mass | 454.65 g/mol |
| 3D model (Jmol) | Interactive image |
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Ezlopitant (INN,[1] code name CJ-11,974) is an NK1 receptor antagonist.[2][3][4] It has antiemetic and antinociceptive effects.[5][6] Pfizer was developing ezlopitant for the treatment of irritable bowel syndrome but it appears to have been discontinued.[2]
See also
- NK1 receptor antagonist
- Maropitant (tert-butyl instead of isopropyl)
References
- 1 2 "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 44" (PDF). World Health Organization. pp. 194–5. Retrieved 17 November 2016.
- 1 2 Evangelista S (October 2001). "Eziopitant. Pfizer". Current Opinion in Investigational Drugs (London, England : 2000). 2 (10): 1441–3. PMID 11890362.
- ↑ Diemunsch P, Grélot L (September 2000). "Potential of substance P antagonists as antiemetics". Drugs. 60 (3): 533–46. doi:10.2165/00003495-200060030-00002. PMID 11030465.
- ↑ Giardina GA, Gagliardi S, Martinelli M (August 2003). "Antagonists at the neurokinin receptors--recent patent literature". IDrugs : the Investigational Drugs Journal. 6 (8): 758–72. PMID 12917772.
- ↑ Tsuchiya M, Fujiwara Y, Kanai Y, et al. (November 2002). "Anti-emetic activity of the novel nonpeptide tachykinin NK1 receptor antagonist ezlopitant (CJ-11,974) against acute and delayed cisplatin-induced emesis in the ferret". Pharmacology. 66 (3): 144–52. doi:10.1159/000063796. PMID 12372904.
- ↑ Tsuchiya M, Sakakibara A, Yamamoto M (January 2005). "A tachykinin NK1 receptor antagonist attenuates the 4 beta-phorbol-12-myristate-13-acetate-induced nociceptive behaviour in the rat". European Journal of Pharmacology. 507 (1-3): 29–34. doi:10.1016/j.ejphar.2004.11.028. PMID 15659291.
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